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Anthony Polverino

Explore the profile of Anthony Polverino including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 13
Citations 271
Followers 0
Related Specialties
Oncology
Biochemistry
Chemistry
Top 10 Co-Authors
Angela Coxon
James Bready
Vinod F Patel
Ling Wang
Richard Kendall
Sean Caenepeel
Paul Rose
Paul Gallant
Yan Gu
Joseph L Kim
Published In
Bioorg Med Chem Lett
J Med Chem
Clin Cancer Res
Cancer Res
J Clin Oncol
Affiliations
Soon will be listed here.
Recent Articles
1.
Antitumor activity of motesanib alone and in combination with cisplatin or docetaxel in multiple human non-small-cell lung cancer xenograft models
Coxon A, Ziegler B, Kaufman S, Xu M, Wang H, Weishuhn D, et al.
Mol Cancer . 2012 Sep; 11:70. PMID: 22992329
Background: Non-small-cell lung cancer (NSCLC) is categorized into various histologic subtypes that play an important role in prognosis and treatment outcome. We investigated the antitumor activity of motesanib, a selective...
2.
Motesanib inhibits Kit mutations associated with gastrointestinal stromal tumors
Caenepeel S, Renshaw-Gegg L, Baher A, Bush T, Baron W, Juan T, et al.
J Exp Clin Cancer Res . 2010 Jul; 29:96. PMID: 20633291
Background: Activating mutations in Kit receptor tyrosine kinase or the related platelet-derived growth factor receptor (PDGFR) play an important role in the pathogenesis of gastrointestinal stromal tumors (GIST). Methods: This...
3.
Augmentation of radiation response by motesanib, a multikinase inhibitor that targets vascular endothelial growth factor receptors
Kruser T, Wheeler D, Armstrong E, Iida M, Kozak K, van der Kogel A, et al.
Clin Cancer Res . 2010 May; 16(14):3639-47. PMID: 20507929
Background: Motesanib is a potent inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, platelet-derived growth factor receptor, and Kit receptors. In this report we examine the...
4.
Broad antitumor activity in breast cancer xenografts by motesanib, a highly selective, oral inhibitor of vascular endothelial growth factor, platelet-derived growth factor, and Kit receptors
Coxon A, Bush T, Saffran D, Kaufman S, Belmontes B, Rex K, et al.
Clin Cancer Res . 2009 Jan; 15(1):110-8. PMID: 19118038
Purpose: Angiogenesis plays a critical role in breast cancer development and progression. Vascular endothelial growth factor (VEGF) is a potent angiogenic factor that regulates endothelial cell proliferation and survival. We...
5.
Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors
Bauer D, Whittington D, Coxon A, Bready J, Harriman S, Patel V, et al.
Bioorg Med Chem Lett . 2008 Aug; 18(17):4844-8. PMID: 18682324
A novel class of potent and selective inhibitors of KDR incorporating an indazole moiety 1 is reported. The discovery, synthesis, and structure-activity relationships of this series of inhibitors have been...
6.
Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties
Choquette D, Teffera Y, Polverino A, Harmange J
Bioorg Med Chem Lett . 2008 Jun; 18(14):4054-8. PMID: 18573658
1,2,3,4-Tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones were identified as potent and selective inhibitors of KDR. The discovery, synthesis, and structure-activity relationships of these novel inhibitors are reported. In vitro metabolism and pharmacokinetic profiles...
7.
Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr
Dominguez C, Smith L, Huang Q, Yuan C, Ouyang X, Cai L, et al.
Bioorg Med Chem Lett . 2007 Sep; 17(21):6003-8. PMID: 17869515
Inhibition of tumor-induced angiogenesis is a promising strategy in anticancer research. Neovascularization is a process required for both tumor growth and metastasis. Enhanced understanding of the underlying molecular mechanisms has...
8.
Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors
Potashman M, Bready J, Coxon A, DeMelfi Jr T, DiPietro L, Doerr N, et al.
J Med Chem . 2007 Aug; 50(18):4351-73. PMID: 17696416
Inhibition of the VEGF signaling pathway has become a valuable approach in the treatment of cancers. Guided by X-ray crystallography and molecular modeling, a series of 2-aminobenzimidazoles and 2-aminobenzoxazoles were...
9.
Safety, pharmacokinetics, and efficacy of AMG 706, an oral multikinase inhibitor, in patients with advanced solid tumors
Rosen L, Kurzrock R, Mulay M, Van Vugt A, Purdom M, Ng C, et al.
J Clin Oncol . 2007 Jun; 25(17):2369-76. PMID: 17557949
Purpose: AMG 706 is an investigational, orally bioavailable inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, platelet-derived growth factor receptor, and stem-cell factor receptor. This phase I,...
10.
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors
Hodous B, Geuns-Meyer S, Hughes P, Albrecht B, Bellon S, Caenepeel S, et al.
Bioorg Med Chem Lett . 2007 Mar; 17(10):2886-9. PMID: 17350837
A novel class of selective Tie-2 inhibitors was derived from a multi-kinase inhibitor 1. By reversing the amide connectivity and incorporating aminotriazine or aminopyridine hinge-binding moieties, excellent Tie-2 potency and...